Capturing Biological Activity in New Heterocyclic Carboxylic ?,?-diaminoesters by Chemical Synthesis

Amino acid derivatives are an important group of peptidomimetics. They exhibit several applications in medicinal chemistry. The amino acids were used as starting keys for synthesis peptides, are known to contribute to various chemotherapeutic effects, as antileukemic, antitumor, antimicrobial , and antiviral agents. Heterocyclic α-amino acids frameworks constitute an essential pharmacophore in many naturally occurring and biologically active agents. In continuation of our ongoing research, this work deals to describe the synthesis and design of carboxylic α,α-diaminoesters through N- alkylation of methyl α-azido glycinate N- benzoylated by different functionalized amines. The structure of the title compound was determined by usual spectroscopic techniques, such as NMR, MS, elemental analysis and corroborated by X-ray crystallography. In this study, we used the modified resazurin microtiter plate assay it is a dye used as an oxidation-reduction indicator in bacterial cell viability assays to evaluate the antimicrobial activity of synthesized products. The results from the disc diffusion assay indicated that the tested compound showed important antibacterial activity against Gram-positive bacteria (IZ 08) and Gram-negative bacteria (IZ 08-10).

Author(s): Karai Oumaima *, A. Alami, H. Faraj, A. El Hallaoui, M. Boukssaim

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